Andrographolide-loaded polymerized phenylboronic acid nanoconstruct for stimuli-responsive chemotherapy

Area of Science:

• Natural Product Chemistry
• Nanotechnology
• Drug Delivery

Background:

• Natural products like andrographolide (AND) show anticancer potential but face solubility challenges for clinical use.
• Overcoming poor aqueous solubility is crucial for effective systemic administration of natural anticancer agents.
• Previous research highlighted the need for advanced delivery systems for compounds like AND.

Purpose of the Study:

• To develop a water-soluble nanoconstruct for improved delivery of andrographolide (AND).
• To create a system that enables controlled release of AND based on intracellular conditions.
• To evaluate the tumor-targeting capabilities and in vivo efficacy of the novel nanoconstruct.

Main Methods:

• Formulation of a water-soluble nanoconstruct via boronic ester linkage between AND and polymerized phenylboronic acid (pPBA).
• Investigated pH- and ATP-dependent release mechanisms of AND from the nanoconstruct.
• Assessed in vitro and in vivo tumor targeting and anticancer efficacy of the pPBA-AND nanoconstruct.

Main Results:

• Successfully formulated a water-soluble pPBA-AND nanoconstruct.
• Demonstrated controlled release of AND triggered by intracellular low pH and high ATP levels.
• Exhibited significant tumor targeting ability in vitro and in vivo.
• Observed substantial inhibition of tumor growth in vivo.

Conclusions:

• The developed pPBA-AND nanoconstruct effectively addresses the solubility limitations of andrographolide.
• This strategy provides a versatile platform for delivering various chemotherapeutics, applicable beyond cancer therapy.
• The pH- and ATP-sensitive release mechanism enhances targeted drug delivery and therapeutic outcomes.